Phase I clinical trial of cefditoren pivoxil (ME 1207): pharmacokinetics in healthy volunteers.

Pharmacokinetics of ME1207 were evaluated in 5 groups of healthy adult male volunteers given single preprandial administration of 100, 200 and 300 mg; postprandial administration of 200 mg; and administration of 200 mg every 12 h for 7 consecutive days. Blood drug concentrations were determined by HPLC and bioassay after oral single administration of 100, 200 and 300 mg before meals. Serum concentrations and major pharmacokinetic parameters (Cmax, Tmax, AUC and T1/2 Ke) determined by these two methods were comparable. Cmax and AUC determined by bioassay after postprandial administration were greater than those determined after preprandial administration. Blood concentrations determined 1.5 and 12 h after each administration, during repeated administration of 200 mg every 12 hours for 7 days, were always about 2.5 and 0 mg/l, respectively, indicating that the drug is not accumulated in the body. Within 24 hours after administration of 100, 200 and 300 mg, 19.93 +/- 5.20, 20.24 +/- 3.72 and 21.29 +/- 5.47%, respectively, of the dose were excreted into urine in an unchanged form.